quinpirole [Ligand Id: 2] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL240773 (Quinpirole) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells | B | 4 | pKi | 100000 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| D2 receptor/mGlu5 receptor/D(2) dopamine receptor/Metabotropic glutamate receptor 5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296096] [GtoPdb: 215, 293] [UniProtKB: P14416, P41594] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - |
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Nature (1990) 347: 146-51 [PMID:1975644]; Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822]; Nature (1991) 350: 610-4 [PMID:1840645]; Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990] |
| ChEMBL | Agonist activity at human dopamine D2 receptor /mGluR5a (unknown origin) expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay | F | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2018) 61: 8212-8225 [PMID:30180563] |
| D2 receptor/mGlu5 receptor in Rat [GtoPdb: 215, 293] [UniProtKB: P61169, P31424] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay | B | 4.06 | pKi | 87000 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis | B | 5.06 | pKi | 8700 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells | B | 5.06 | pKi | 8700 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes | B | 4.06 | pKi | 87000 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes | B | 4.14 | pKi | 72000 | nM | Ki | J Med Chem (2009) 52: 6860-6870 [PMID:19807103] |
| Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
| ChEMBL | Inhibition constant against [3H]SCH-23390 binding to Dopamine receptor D1 in bovine striatal membranes | B | 4.7 | pKi | >20000 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Binding affinity (low) towards bovine dopamine receptor 1 by using [3H]-SCH- 23390 (0.3 nM) as radioligand | B | 4.7 | pKi | >20000 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (1990) 33: 1756-1764 [PMID:1971308] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 long receptor expressed in CHO cells; Low binding affinity | B | 4.51 | pKi | 31000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 short receptor expressed in CHO cells; Low binding affinity | B | 5.4 | pKi | 4000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells | B | 5.51 | pKi | 3100 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Binding affinity (low) towards human dopamine receptor 2 (long) against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells | B | 5.51 | pKi | 3100 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | Binding affinity (low) towards human dopamine receptor 2 short against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells | B | 5.52 | pKi | 3000 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D2S expressed in CHO cells | B | 5.52 | pKi | 3000 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 5.53 | pKi | 2950 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Affinity towards Dopamine receptor D2 | B | 5.59 | pKi | 2570 | nM | Ki | J Med Chem (1998) 41: 4385-4399 [PMID:9784114] |
| ChEMBL | Displacement of [3H]YM-09151-2 from human dopamine D2 receptor expressed in CHOp cells | B | 5.93 | pKi | 1185 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2long receptor expressed in CHO cells | B | 6.02 | pKi | 950 | nM | Ki | J Med Chem (2009) 52: 6860-6870 [PMID:19807103] |
| ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2short receptor expressed in CHO cells | B | 6.06 | pKi | 870 | nM | Ki | J Med Chem (2009) 52: 6860-6870 [PMID:19807103] |
| ChEMBL | Displacement of [3H]spiperone from human D2L receptor expressed in CHO cells | B | 6.59 | pKi | 260 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assay | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2L receptor transfected in CHO cells after 1 hr by scintillation counting analysis | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells | B | 7.15 | pKi | 70 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assay | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2S receptor expressed in CHO cells | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2S receptor transfected in CHO cells after 1 hr by scintillation counting analysis | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D2 long in CHO cells | B | 7.19 | pKi | 64 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 851-854 [PMID:12617906] |
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 long receptor expressed in CHO cells; high binding affinity | B | 7.19 | pKi | 64 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 short receptor expressed in CHO cells; high binding affinity | B | 7.28 | pKi | 52 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D2 short in CHO cells | B | 7.28 | pKi | 52 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 851-854 [PMID:12617906] |
| ChEMBL | High binding affinity towards human dopamine receptor 2 (short) expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D2S expressed in CHO cells | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| GtoPdb | - | - | 7.7 | pKi | - | - | - |
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Nature (1990) 347: 146-51 [PMID:1975644]; Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822]; Nature (1991) 350: 610-4 [PMID:1840645]; Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990] |
| ChEMBL | Displacement of [3H]7-OH-DPAT from human dopamine D2L receptor expressed in CHO cells | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis | B | 7.88 | pKi | 13.1 | nM | Ki | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Displacement of [3H]7-OH-DPAT from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 8.25 | pKi | 5.56 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control. | F | 6.34 | pIC50 | 462 | nM | IC50 | US-9359372-B2. Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof (2016) |
| ChEMBL | Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | F | 5.55 | pEC50 | 2800 | nM | EC50 | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | F | 5.57 | pEC50 | 2700 | nM | EC50 | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | F | 5.64 | pEC50 | 2300 | nM | EC50 | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay | F | 5.79 | pEC50 | 1621.81 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay | F | 5.79 | pEC50 | 1621.81 | nM | EC50 | Bioorg Med Chem (2015) 23: 6195-6209 [PMID:26299826] |
| ChEMBL | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay | F | 5.8 | pEC50 | 1600 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay | F | 5.8 | pEC50 | 1600 | nM | EC50 | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Agonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay | F | 6.17 | pEC50 | 680 | nM | EC50 | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
| ChEMBL | Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay | F | 6.21 | pEC50 | 616.6 | nM | EC50 | Bioorg Med Chem (2015) 23: 6195-6209 [PMID:26299826] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay | B | 6.45 | pEC50 | 353.2 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay | F | 6.48 | pEC50 | 330 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-1 recruitment after 15 mins by BRET assay | B | 6.53 | pEC50 | 295 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay | F | 6.57 | pEC50 | 270 | nM | EC50 | J Med Chem (2017) 60: 4693-4713 [PMID:28489379] |
| ChEMBL | Agonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay | F | 6.62 | pEC50 | 240 | nM | EC50 | Bioorg Med Chem (2009) 17: 4873-4880 [PMID:19559623] |
| ChEMBL | Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay | F | 6.64 | pEC50 | 230 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control | F | 6.82 | pEC50 | 151.36 | nM | EC50 | J Nat Prod (2020) 83: 127-133 [PMID:31933369] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-2 recruitment after 15 mins by BRET assay | B | 6.82 | pEC50 | 151 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control | F | 6.82 | pEC50 | 150 | nM | EC50 | J Nat Prod (2020) 83: 127-133 [PMID:31933369] |
| ChEMBL | Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay | B | 6.83 | pEC50 | 147.6 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay | F | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (2011) 54: 7911-7919 [PMID:21999579] |
| ChEMBL | Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay | B | 7.07 | pEC50 | 86 | nM | EC50 | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay | B | 7.08 | pEC50 | 83 | nM | EC50 | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay | B | 7.14 | pEC50 | 73 | nM | EC50 | Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802] |
| ChEMBL | Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay | B | 7.19 | pEC50 | 64 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay | B | 7.28 | pEC50 | 52 | nM | EC50 | J Med Chem (2017) 60: 4693-4713 [PMID:28489379] |
| ChEMBL | Activity at pro-link-tagged D2S-ARMS2PK2 (unknown origin) expressed in HEK293 cells by beta-arrestin-2 recruitment assay | B | 7.29 | pEC50 | 51 | nM | EC50 | Bioorg Med Chem (2015) 23: 6195-6209 [PMID:26299826] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay | B | 7.41 | pEC50 | 38.7 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Agonist activity at human histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay | F | 7.55 | pEC50 | 28.18 | nM | EC50 | Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay | B | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (2017) 60: 4693-4713 [PMID:28489379] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 7.8 | pEC50 | 15.7 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay | F | 7.96 | pEC50 | 10.9 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | B | 8.09 | pEC50 | 8.2 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor | F | 8.12 | pEC50 | 7.6 | nM | EC50 | J Med Chem (1994) 37: 4251-4257 [PMID:7990124] |
| ChEMBL | Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | F | 8.13 | pEC50 | 7.4 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay | B | 8.23 | pEC50 | 5.9 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay | B | 8.29 | pEC50 | 5.1 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Eur J Med Chem (2021) 212: 113151-113151 [PMID:33450620] |
| ChEMBL | Effective dose was measured by the stimulation of mitogenesis at Dopamine receptor D4.2 | B | 8.43 | pEC50 | 3.7 | nM | EC50 | J Med Chem (2000) 43: 4563-4569 [PMID:11087581] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.52 | pEC50 | 3.02 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay | B | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.52 | pEC50 | 2.99 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing Galpahi1/Gbeta1/GFP2-Ggamma2 assessed as Galphai1 dissociation after 15 mins in presence of coelenterazine 400a by luciferase reporter gene assay | B | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2019) 62: 4755-4771 [PMID:30964661] |
| ChEMBL | Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity) | B | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2000) 43: 3549-3557 [PMID:11000009] |
| ChEMBL | Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay | F | 8.74 | pEC50 | 1.82 | nM | EC50 | J Med Chem (2019) 62: 4755-4771 [PMID:30964661] |
| ChEMBL | Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2019) 62: 4755-4771 [PMID:30964661] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2018) 61: 8212-8225 [PMID:30180563] |
| ChEMBL | Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol | F | 8.8 | pEC50 | 1.6 | nM | EC50 | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay | F | 8.89 | pEC50 | 1.3 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay | B | 8.92 | pEC50 | 1.2 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay | B | 8.92 | pEC50 | 1.2 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.93 | pEC50 | 1.18 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.93 | pEC50 | 1.18 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, low affinity site | B | 5.59 | pKi | 2580 | nM | Ki | J Med Chem (1998) 41: 4933-4938 [PMID:9836610] |
| ChEMBL | Tested for binding affinity against Dopamine receptor D2 like from bovine striatum membranes by using [3H]YM-09151-2 radioligand | B | 5.82 | pKi | 1500 | nM | Ki | J Med Chem (1998) 41: 4933-4938 [PMID:9836610] |
| ChEMBL | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, high affinity site | B | 7.23 | pKi | 59.4 | nM | Ki | J Med Chem (1998) 41: 4933-4938 [PMID:9836610] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 5.17 | pKd | 6700 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 5.46 | pKd | 3500 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. | B | 5.64 | pKd | 2300 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. | B | 5.72 | pKd | 1900 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
| ChEMBL | Binding affinity against Dopamine receptor D2 in rat striatal membranes using [3H]spiperone | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2371-2376 |
| ChEMBL | Compound was evaluated for its ability to displace [3H]raclopride from dopamine receptor D2 in rat striatal homogenates | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (1992) 35: 1076-1092 [PMID:1348089] |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 5.32 | pIC50 | 4784 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 5.36 | pIC50 | 4321 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Displacement of [3H]- -spiperone from Dopamine receptor D2 in rat striatum | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1990) 33: 1756-1764 [PMID:1971308] |
| ChEMBL | Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | B | 7.32 | pEC50 | 48 | nM | EC50 | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Effective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | B | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | F | 8.05 | pEC50 | 9 | nM | EC50 | J Med Chem (2006) 49: 6848-6857 [PMID:17154515] |
| ChEMBL | Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat | F | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2000) 43: 2871-2882 [PMID:10956195] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Low binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | B | 6.38 | pKi | 420 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells | B | 6.38 | pKi | 420 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | In vitro for its ability to displace [3H]- spiperoneI from cloned human Dopamine receptor D3 expressed in CHO cells; Low binding affinity | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Tested for the ability to displace [125I]iodosulpiride from human cloned Dopamine receptor D3, expressed in CHO cells | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2715-2720 [PMID:10509922] |
| ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO cells | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (2009) 52: 6860-6870 [PMID:19807103] |
| ChEMBL | Displacement of [3H]YM-09151-2 from human dopamine D3 receptor expressed in CHOp cells | B | 7.37 | pKi | 43 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 7.53 | pKi | 29.3 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | High binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D3 in CHO cells | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 851-854 [PMID:12617906] |
| ChEMBL | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D3 expressed in CHO cells; high binding affinity | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells | B | 7.62 | pKi | 23.99 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells by competitive binding assay | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor transfected in CHO cells after 1 hr by scintillation counting analysis | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor by liquid scintillation counting | B | 7.9 | pKi | 12.5 | nM | Ki | Bioorg Med Chem (2009) 17: 758-766 [PMID:19081257] |
| GtoPdb | - | - | 8 | pKi | 10 | nM | Ki |
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822]; J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180]; Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990]; Neuroreport (1995) 6: 329-332 [PMID:7756621]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Nature (1990) 347: 146-51 [PMID:1975644]; Nature (1991) 350: 610-4 [PMID:1840645] |
| ChEMBL | Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 8.1 | pKi | 8.01 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D3 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis | B | 8.17 | pKi | 6.76 | nM | Ki | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
| ChEMBL | Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay | F | 6.73 | pEC50 | 186.3 | nM | EC50 | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| ChEMBL | Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay | B | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2020) 63: 4579-4602 [PMID:32282200] |
| ChEMBL | Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay | F | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
| ChEMBL | Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem (2015) 23: 3938-3947 [PMID:25564378] |
| ChEMBL | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | F | 8.01 | pEC50 | 9.77 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | F | 8.01 | pEC50 | 9.7 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay | F | 8.08 | pEC50 | 8.4 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs | F | 8.28 | pEC50 | 5.2 | nM | EC50 | Bioorg Med Chem (2007) 15: 7248-7257 [PMID:17827018] |
| ChEMBL | Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | F | 8.47 | pEC50 | 3.4 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.48 | pEC50 | 3.31 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.48 | pEC50 | 3.31 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | B | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells | F | 8.51 | pEC50 | 3.1 | nM | EC50 | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay | B | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay | B | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2019) 62: 5132-5147 [PMID:31021617] |
| ChEMBL | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay | F | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| ChEMBL | Effective concentration against dopamine D3 receptor | B | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay | F | 8.62 | pEC50 | 2.4 | nM | EC50 | Bioorg Med Chem (2015) 23: 3938-3947 [PMID:25564378] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay | F | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| ChEMBL | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay | B | 8.68 | pEC50 | 2.1 | nM | EC50 | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.71 | pEC50 | 1.97 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.71 | pEC50 | 1.95 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay | F | 8.75 | pEC50 | 1.78 | nM | EC50 | Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637] |
| ChEMBL | Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity) | B | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (2000) 43: 3549-3557 [PMID:11000009] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2670-2674 [PMID:21273071] |
| ChEMBL | Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor | F | 8.85 | pEC50 | 1.4 | nM | EC50 | J Med Chem (2005) 48: 3696-3699 [PMID:15916420] |
| ChEMBL | Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay | F | 9.38 | pEC50 | 0.42 | nM | EC50 | J Med Chem (2020) 63: 4579-4602 [PMID:32282200] |
| ChEMBL | Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay | F | 10.01 | pEC50 | 0.1 | nM | EC50 | Medchemcomm (2018) 9: 1457-1465 [PMID:30288220] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; Nature (1990) 347: 146-51 [PMID:1975644] |
| ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 8.25 | pKi | 5.65 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 7.54 | pIC50 | 29 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 7.6 | pIC50 | 25 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Basal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligand | B | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| ChEMBL | Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (2000) 43: 2871-2882 [PMID:10956195] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity | B | 7.28 | pKi | 53 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells | B | 7.28 | pKi | 53 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | B | 7.28 | pKi | 53 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Nature (1991) 350: 610-4 [PMID:1840645]; Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990] |
| ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2009) 52: 6860-6870 [PMID:19807103] |
| ChEMBL | Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells | B | 8.07 | pKi | 8.5 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 851-854 [PMID:12617906] |
| ChEMBL | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay | B | 7.08 | pEC50 | 83 | nM | EC50 | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor | F | 7.31 | pEC50 | 49 | nM | EC50 | J Med Chem (2005) 48: 3696-3699 [PMID:15916420] |
| ChEMBL | Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding | F | 7.31 | pEC50 | 49 | nM | EC50 | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
| ChEMBL | Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis | F | 7.51 | pEC50 | 31 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay | F | 7.64 | pEC50 | 23 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2 | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2005) 48: 3696-3699 [PMID:15916420] |
| ChEMBL | Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | F | 7.96 | pEC50 | 11 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor | B | 8 | pEC50 | 9.9 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 851-854 [PMID:12617906] |
| ChEMBL | Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | B | 8.06 | pEC50 | 8.7 | nM | EC50 | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2006) 49: 6848-6857 [PMID:17154515] |
| ChEMBL | Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay | F | 8.57 | pEC50 | 2.7 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| ChEMBL | Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay | F | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Effective concentration of compound required against human Dopamine D4.2 receptor | F | 8.66 | pEC50 | 2.2 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813] |
| ChEMBL | Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| ChEMBL | Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay | F | 8.85 | pEC50 | 1.4 | nM | EC50 | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor transfected in HEK293 cells by scintillation counting analysis | B | 4.6 | pKi | 25000 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
